AZD 5438 CAS: 602306-29-6
MF: C18H21N5O2S
MW: 371.46

AZD 5438 (CAS 602306-29-6)

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Alternate Names: AZD 5438 is also known as 4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine and N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine
Application AZD 5438 is an antiproliferative agent and potent inhibitor of cyclin-dependent kinases Cdk1, Cdk2, and Cdk9
CAS 등록번호: 602306-29-6
순도: ≥98%
분자량: 371.46
분자식: C18H21N5O2S
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
* 참조분석증명서대량의 측정 데이터(함수량포함).
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AZD 5438 is an antiproliferative agent and potent inhibitor of cyclin-dependent kinases Cdk1/cyclin B1 (IC50 = 16 nM), Cdk2/cyclin E (IC50 = 6 nM), Cdk2/cyclin A (IC50 = 45 nM), Cdk6/cyclin D3 (IC50 = 21 nM), and Cdk9/cyclin T (IC50 = 20 nM). AZD 5438 also inhibits the kinase activity of p25-cdk5 (IC50 = 14 nM) and glycogen synthase kinase 3β (IC50 = 17 nM). AZD 5438 induces cell cycle arrest by inhibiting phosphorylation of cdk-dependent substrates, and exhibits the broad antiproliferative activity against a range of tumor cell lines including lung, colorectal, breast, prostate, and hematologic tumors with IC50 ranging from 0.2 μM (MCF-7) to 1.7 μM (ARH-77).


References

1. Camidge, D.R. et al. 2007. Cancer Chemother. Pharmacol. 60(3): 391-398. PMID: 17115157
2. Camidge, D.R. et al. 2007. Cancer Chemother. Pharmacol. 60(4): 479-488. PMID: 17143601
3. Dickson, M.A. and Schwartz, G.K. 2009. Curr Oncol. 16(2): 36-43. PMID: 19370178
4. Byth, K.F. et al. 2009. Mol. Cancer Ther. 8(7): 1856-1866. PMID: 19509270
5. Boss, D.S. et al. 2010. Ann. Oncol. 21(4): 884-894. PMID: 19825886
6. Raghavan, P. et al. 2012. Int J Radiat Oncol Biol Phys. PMID: 22795803

Physical State :
Solid
용해도 :
Soluble in DMSO (100 mM), water (<1 mg/ml) at 25° C, and ethanol (74 mg/ml) at 25° C.
저장 :
Desiccate at room temperature
녹는점 :
246.01° C (Predicted)
비등점 :
655.2±65.0° C at 760 mmHg
밀도 :
1.3±0.1 g/cm3
굴절률 :
n20D 1.65 (Predicted)
IC50 :
cyclin-dependent kinase (cdk)1: IC50 = 16 nM; cyclin-dependent kinase (cdk)2: IC50 = 6 nM; cyclin-dependent kinase (cdk)9: IC50 = 20 nM; kinase activity of p25-cdk5: IC50 = 14 nM; glycogen synthase kinase 3β: IC50 = 17 nM; antiproliferative activity: IC50 = 0.2 µM (MCF-7); antiproliferative activity: IC50 = 1.7 µM (ARH-77); Cyclin T1: IC50 = 20 nM (human); G1/S-specific cyclin D3: IC50 = 21 nM (human); Cyclin A2: IC50 = 45 nM (human)
pK Values :
pKb: 4.08 (Predicted)
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
PubChem CID :
MDL Number :
MFCD11112135
SMILES :
CC1=NC=C(N1C(C)C)C2=NC(=NC=C2)NC3=CC=C(C=C3)S(=O)(=O)C

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